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Diflunisal solid dispersion and preparation method thereof

A technology of solid dispersion and diflunisal, applied in the field of medicine, can solve the problems of limited wide application, thermal decomposition of drugs and carriers, etc., and achieve the effects of reducing the dosage, increasing the solubility, and having no solvent residue.

Active Publication Date: 2013-07-17
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, for drugs and carriers with higher melting points, the melting method and hot-melt extrusion method easily lead to thermal decomposition of drugs and carriers, which limits the wide application of this method

Method used

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  • Diflunisal solid dispersion and preparation method thereof
  • Diflunisal solid dispersion and preparation method thereof
  • Diflunisal solid dispersion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] In this embodiment, a solid dispersion of diflunisal is prepared from diflunisal and Soluplus as active ingredients, and Soluplus accounts for 80% by mass of the solid dispersion of diflunisal.

[0044] Take 2g of diflunisal, 8g of Soluplus, and mix well. Set the extrusion temperature of the twin-screw hot-melt extruder to be 160 ° C, start the screw after reaching the preset temperature, the screw speed is 150 rpm, and the physical mixture made is added to the extruder, and the mixture passes through the screw to form strips shape extrusion; the hot-melt extruded strips are crushed and passed through an 80-mesh sieve to obtain diflunisal solid dispersion powder.

[0045] The solid dispersion powder X-ray diffraction that present embodiment prepares ( figure 1 ) shows that the drug is dispersed in the carrier material in an amorphous or molecular state. The results of high-performance liquid chromatography showed that the drug content and related substances had no obv...

Embodiment 2

[0047] In this embodiment, a diflunisal solid dispersion is prepared from diflunisal and copovidone VA64 as active ingredients, and the mass percentage of copovidone VA64 in the diflunisal solid dispersion is 70% %.

[0048] Take 3g of diflunisal and 7g of copovidone VA64 (PVPVA64), and mix them evenly. Set the extrusion temperature of the twin-screw hot-melt extruder to be 100°C, start the screw after reaching the preset temperature, the screw speed is 50 rpm, and the physical mixture made is added to the extruder, and the mixture passes through the screw to form strips shape extrusion; the hot-melt extruded strips are crushed and passed through an 80-mesh sieve to obtain diflunisal solid dispersion powder.

[0049] The present embodiment obtains powder X-ray diffraction ( image 3 ) shows that the drug is dispersed in the carrier material in an amorphous or molecular state. The results of high-performance liquid chromatography showed that the drug content and related subs...

Embodiment 3

[0051] In this embodiment, a diflunisal solid dispersion is prepared from diflunisal and copovidone VA64 as active ingredients, and the mass percentage of copovidone VA64 in the diflunisal solid dispersion is 70% %.

[0052] Take 3g of diflunisal and 7g of copovidone VA64 (PVPVA64), and mix them evenly. Set the extrusion temperature of the twin-screw hot-melt extruder to be 140 ° C, start the screw after reaching the preset temperature, the screw speed is 250 rpm, and the physical mixture made is added to the extruder, and the mixture passes through the screw to form strips shape extrusion; the hot-melt extruded strips are crushed and passed through an 80-mesh sieve to obtain a drug solid dispersion powder.

[0053] The present embodiment prepares solid dispersion powder X-ray diffraction ( Figure 5 ) shows that the drug is dispersed in the carrier material in an amorphous or molecular state. The results of high-performance liquid chromatography showed that the drug conten...

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Abstract

The invention discloses a diflunisal solid dispersion and a preparation method thereof. The solid dispersion is composed of diflunisal as active components and high-polymer carrier materials. The high-polymer carrier materials are 40-90% of the diflunisal in total and selected from povidones, copovidones, and polyethylene glycol / vinyl caprolactam / vinyl acetate copolymer or hydroxypropyl methylcellulose. The preparation method adopts a hot-melting extrusion method. The diflunisal solid dispersion obtained is higher in solubility and quick and high in dissolving, bioavailability of indissolvable drugs is improved, drug dosage is reduced, and adverse drug reaction is reduced.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a diflunisal solid dispersion and a preparation method thereof. Background technique [0002] The solubility of a drug in solution is a fundamental parameter for preparation of formulations, directly affects the absorption of the drug and affects the bioavailability of the drug. With the widespread application of combinatorial chemistry and high-throughput screening in the development of new drugs, at present, reports indicate that 35%-40% of newly discovered drugs are seriously affected by their low solubility or low permeability in their effective absorption in the gastrointestinal tract , and may result in lower bioavailability. Therefore, it has become one of the biggest challenges for pharmaceutical researchers to improve the solubility and dissolution rate of poorly soluble drugs by means of formulations and methods, thereby improving their bioavailability and clinical ef...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/603A61K47/32A61K47/34A61K47/38A61P29/00
Inventor 吴传斌陆明郭喆霏
Owner SUN YAT SEN UNIV
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